Costa Eliatania Clementino, Menezes Pedro Modesto Nascimento, de Almeida Ricardo Lúcio, Silva Fabrício Souza, de Araújo Ribeiro Luciano Augusto, da Silva James Amalda, de Oliveira Ana Paula, da Cruz Araújo Edigênia Cavalcante, Rolim Larissa Araújo, Nunes Xirley Pereira
Rede Nordeste de Biostecnologia (RENORBIO), Universidade Federal Rural de Pernambuco (UFRPE), Recife, PE, Brazil.
Pós-graduação em Biociências (PGB), Universidade Federal do Vale do São Francisco (UNIVASF), Petrolina, PE, Brazil.
Heliyon. 2020 Dec 1;6(12):e05461. doi: 10.1016/j.heliyon.2020.e05461. eCollection 2020 Dec.
The study aimed to include the isolated vitexin of in the β-cyclodextrin cavity to improve the solubility of this flavone. Its characterization was performed by techniques such as H NMR/ROESY (Nuclear Magnetic Resonance Spectroscopy), FT-IR (Infrared Spectroscopy with Fourier Transform), SEM (Morphological analysis of IC by Scanning Electron Microscopy) and dissolution study . In addition, the following activities were evaluated in the animal models: expectorant, phenol red dosage in bronchoalveolar lavage and antitussive, cough induced by citric acid. In the characterization of the complex, interaction between hydrogens of ring B of vitexin and (H3) of β-CD was observed, in addition to changes in morphology. In the dissolution test, an increase in the rate of dissolution of vitexin was observed in the first 30 min for the CI vitexin/β-CD when compared with vitexin. Regarding the pharmacological activity, it was observed that the inclusion complex (IC) vitexin/β-CD in the equivalent doses of 0.2, 1 and 5 mg/kg of flavone presented higher expectorant activity when compared to vitexin (p < 0.05), suggesting increased bioavailability. As for the antitussive activity, both vitexin and the complex had similar effects and were dose independent. In the toxicity test using , vitexin and IC vitexin/β-CD were considered non-toxic. At last, the study efficacy of vitexin/β-CD IC as an expectorant and of vitexin as antitussive. All of these data are being described for the first time.
该研究旨在将异牡荆素包合于β-环糊精腔内，以提高这种黄酮的溶解度。通过核磁共振氢谱/旋转坐标系二维核磁共振谱（NMR）、傅里叶变换红外光谱（FT-IR）、扫描电子显微镜（SEM）对包合物进行形态分析以及溶出度研究等技术对其进行表征。此外，还在动物模型中评估了以下活性：祛痰作用，通过支气管肺泡灌洗中的酚红剂量评估；镇咳作用，通过柠檬酸诱导咳嗽评估。在包合物的表征中，除了形态变化外，还观察到异牡荆素B环上的氢与β-环糊精的（H3）之间存在相互作用。在溶出度试验中，与异牡荆素相比，包合物异牡荆素/β-环糊精在最初30分钟内异牡荆素的溶出速率有所增加。关于药理活性，观察到在黄酮等效剂量为0.2、1和5mg/kg时，异牡荆素/β-环糊精包合物（IC）与异牡荆素相比具有更高的祛痰活性（p<0.05），表明生物利用度增加。至于镇咳活性，异牡荆素和包合物具有相似的效果且与剂量无关。在使用……的毒性试验中，异牡荆素和异牡荆素/β-环糊精包合物被认为无毒。最后，该研究表明异牡荆素/β-环糊精包合物具有祛痰作用，异牡荆素具有镇咳作用。所有这些数据均为首次报道。
